Injectable formulation

Abstract

An object of the present invention is to provide a sustained-release injectable preparation which is in a medication administration form that can provide the effect of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one for a prolonged period of time, the preparation releasing a therapeutically effective amount of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one for at least one week. The present invention provides an injectable preparation containing 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof as an active ingredient, which releases the active ingredient in such a manner that its blood concentration is maintained for at least one week.

The invention claimed is: 
     
       1. An injectable preparation comprising 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof, particle binders, and water for injection, the particle binders being sodium chloride and at least one member selected from the group consisting of polyoxyethylene sorbitan fatty acid esters and polyethylene glycols,
 wherein the 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof is a dihydrate of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one. 
 
     
     
       2. The injectable preparation according to  claim 1 , wherein secondary particles are formed by the aggregation of particles (primary particles) of the 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof, and the secondary particles have a mean-particle diameter (a mean secondary particle diameter) of 4 to 17 μm. 
     
     
       3. The injectable preparation according to  claim 1  or  2 , having a pH of 5 to 8. 
     
     
       4. A prefilled syringe that is prefilled with the injectable preparation according to  claim 1  or  2 . 
     
     
       5. The injectable preparation according to  claim 1  or  2 , wherein the particle binders are sodium chloride and a polyethylene glycol. 
     
     
       6. The injectable preparation according to  claim 5 , wherein the polyethylene glycol is macrogol 400 or macrogol 4000. 
     
     
       7. The injectable preparation according to  claim 5 , further comprising a polyoxyethylene sorbitan fatty acid ester. 
     
     
       8. The injectable preparation according to  claim 7 , wherein the polyoxyethylene sorbitan fatty acid ester is polyoxyethylene (20) sorbitan oleate. 
     
     
       9. The injectable preparation according to  claim 2 , wherein the particles of 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof have a mean primary particle diameter of 1 to 10 μm. 
     
     
       10. The injectable preparation according to  claim 1  or  2 , wherein the preparation releases an active ingredient in such a manner that its therapeutically effective blood concentration is maintained for at least one week. 
     
     
       11. A method for treating schizophrenia, bipolar disorder, or depression, the method comprising administering an effective amount of the injectable preparation according to  claim 1  or  2 . 
     
     
       12. The method according to  claim 11 , wherein the preparation is administered intramuscularly or subcutaneously. 
     
     
       13. A method for releasing an active ingredient in such a manner that its therapeutically effective blood concentration is maintained for at least one week comprising administering the injectable preparation according to  claim 1  or  2 .